AZD-3043: A novel, metabolically labile sedative-hypnotic agent with rapid and predictable emergence from hypnosis

Anesthesiology

Volumn 116, Issue 6, 2012, Pages 1267-1277

  Egan, Talmage D ^a   Obara, Shinju ^a   Jenkins, Thomas E ^b   Jaw Tsai, Sarah S ^b   Amagasu, Shanti ^b   Cook, Daniel R ^c   Steffensen, Scott C ^d   Beattie, David T ^b  

^a UNIVERSITY OF UTAH SCHOOL OF MEDICINE   (United States)

^b THERAVANCE INC   (United States)

^c NeuroInsight LLC   (United States)

^d BRIGHAM YOUNG UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; AZD 3043; CHLORIDE; ESTER DERIVATIVE; FENTANYL; HYPNOTIC SEDATIVE AGENT; PROPANIDID; PROPOFOL; PROPRANOLOL; RADIOLIGAND; REMIFENTANIL; TERT BUTYLBICYCLOPHOSPHOROTHIOATE S 35;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BLOOD SAMPLING; BRAIN CELL; CHLORIDE CURRENT; COMPUTER SIMULATION; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFECT; DRUG HYDROLYSIS; DRUG STABILITY; ELECTROENCEPHALOGRAPHY; FEMALE; HYPNOSIS; IN VITRO STUDY; LIGAND BINDING; LIVER MICROSOME; MALE; METABOLISM; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BINDING; RIGHTING REFLEX;

ANESTHESIA RECOVERY PERIOD; ANIMALS; CHEMISTRY, PHARMACEUTICAL; COMPUTER SIMULATION; CONSCIOUS SEDATION; ELECTROENCEPHALOGRAPHY; FEMALE; HYPNOTICS AND SEDATIVES; INFUSIONS, INTRAVENOUS; MALE; MICROSOMES, LIVER; PATCH-CLAMP TECHNIQUES; PHENYLACETATES; PREGNANCY; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A; SWINE; SWINE, MINIATURE;

EID: 84861597092     PISSN: 00033022     EISSN: 15281175     Source Type: Journal    
DOI: 10.1097/ALN.0b013e31825685a6     Document Type: Article

References (21)

1. Peduto VA, Concas A, Santoro G, Biggio G, Gessa GL: Biochemical and electrophysiologic evidence that propofol enhances GABAergic transmission in the rat brain. ANESTHESIOLOGY 1991; 75:1000-9
2. A receptors, The GABA Receptors. Edited by Enna SJ, Bowery NG. Totowa, New Jersey, Humana Press Inc, 1997, pp 121-56
3. Shafer A, Doze VA, Shafer SL, White PF: Pharmacokinetics and pharmacodynamics of propofol infusions during general anesthesia. ANESTHESIOLOGY 1988; 69:348-56
4. Gunner BW, Harrison GA, Walker WD, Jenkinson IS: Propanidid, a new short-acting anaesthetic. Med J Aust 1965; 2:327-9
5. Habazettl H, Vollmar B, Rohrich F, Conzen P, Doenicke A, Baethmann A: [Anesthesiologic efficacy of propanidid as a liposome dispersion. An experimental study with rats]. Anaesthesist 1992; 41:448-56
6. Glen JB, Hunter SC: Pharmacology of an emulsion formulation of ICI 35 868. Br J Anaesth 1984; 56:617-26
7. Lindsay RM, Evison CJ, Winter J: Culture of adult mammalian peripheral neurons, Cellular Neurobiology: A Practical Approach. New York, Oxford University Press, 1991, pp 3-17
8. Lingamaneni R, Krasowski MD, Jenkins A, Truong T, Giunta AL, Blackbeer J, MacIver MB, Harrison NL, Hemmings HC Jr: Anesthetic properties of 4-iodopropofol: Implications for mechanisms of anesthesia. ANESTHESIOLOGY 2001; 94:1050-7
9. Steffensen SC, Lee RS, Henriksen SJ, Packer TL, Cook DR: A novel electroencephalographic analysis method discriminates alcohol effects from those of other sedative/hypnotics. J Neurosci Methods 2002; 115:145-56
10. Ko JC, Williams BL, Smith VL, McGrath CJ, Jacobson JD: Comparison of Telazol, Telazol-ketamine, Telazol-xylazine, and Telazol-ketamine-xylazine as chemical restraint and an-esthetic induction combination in swine. Lab Anim Sci 1993; 43:476-80
11. Varvel JR, Donoho DL, Shafer SL: Measuring the predictive performance of computer-controlled infusion pumps. J Pharmacokinet Biopharm 1992; 20:63-94
12. Holford NH, Sheiner LB: Understanding the dose-effect relationship: Clinical application of pharmacokinetic-pharmacodynamic models. Clin Pharmacokinet 1981; 6:429-53
13. Johnson KB, Egan TD, Kern SE, White JL, McJames SW, Syroid N, Whiddon D, Church T: The influence of hemorrhagic shock on propofol: A pharmacokinetic and pharmacodynamic analysis. ANESTHESIOLOGY 2003; 99:409-20
14. Youngs EJ, Shafer SL: Pharmacokinetic parameters relevant to recovery from opioids. ANESTHESIOLOGY 1994; 81:833-42
15. Lin LH, Chen LL, Zirrolli JA, Harris RA: General anesthetics potentiate gamma-aminobutyric acid actions on gamma-aminobutyric acidA receptors expressed by Xenopus oocytes: Lack of involvement of intracellular calcium. J Pharmacol Exp Ther 1992; 263:569-78
16. A-receptor subtypes really occur in the brain? Trends Neurosci 1996; 19:139-43
17. Avramov MN, White PF: Use of alfentanil and propofol for outpatient monitored anesthesia care: Determining the optimal dosing regimen. Anesth Analg 1997; 85:566-72
18. Egan TD: Is Anesthesiology going soft?: Trends in fragile pharmacology. ANESTHESIOLOGY 2009; 111:229-30
19. Sneyd JR, Rigby-Jones AE: New drugs and technologies, intravenous anaesthesia is on the move (again). Br J Anaesth 2010; 105:246-54
20. Kilpatrick GJ, McIntyre MS, Cox RF, Stafford JA, Pacofsky GJ, Lovell GG, Wiard RP, Feldman PL, Collins H, Waszczak BL, Tilbrook GS: CNS 7056: A novel ultra-short-acting Benzodiazepine. ANESTHESIOLOGY 2007; 107:60-6
21. Cotten JF, Husain SS, Forman SA, Miller KW, Kelly EW, Nguyen HH, Raines DE: Methoxycarbonyl-etomidate: A novel rapidly metabolized and ultra-short-acting etomidate analogue that does not produce prolonged adrenocortical suppression. ANESTHESIOLOGY 2009; 111:240-9